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Pharmacology Mentor > Blog > Pharmacology > ANS > Parasympatholytics/Cholinergic antagonists
ANSPharmacology

Parasympatholytics/Cholinergic antagonists

Last updated: 2024/03/25 at 1:04 AM
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Cholinergic antagonists - Parasympatholytics
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Introduction

Parasympatholytics, also known as anticholinergics, are a class of drugs that inhibit the actions of the neurotransmitter acetylcholine on parasympathetic nerve endings. These drugs can be classified based on their mode of action and target sites. This article will delve into the classification of parasympatholytics, individual drug pharmacological actions, clinical uses, adverse effects, atropine poisoning, contraindications, and other important information.

Contents
IntroductionClassification of ParasympatholyticsAntimuscarinic agentsGanglionic blockersIndividual Drug Pharmacological ActionsAtropineScopolamineGlycopyrrolateMecamylaminePharmacological ActionsCentral Nervous SystemPeripheral Nervous SystemUsesAnesthetic Pre-treatmentOphthalmologyAntispasmodicBradycardiaOrganophosphate Poisoning (OP Poisoning)ContraindicationsGlaucomaProstatic HypertrophyIntestinal ObstructionMyasthenia GravisTachycardiaAdverse EffectsAtropine PoisoningConclusion

Classification of Parasympatholytics

Parasympatholytics can be broadly classified into two groups:

Antimuscarinic agents

These agents block the action of acetylcholine on muscarinic receptors, which are found in smooth muscle, cardiac muscle, and glandular tissue. Examples include atropine, scopolamine, and glycopyrrolate.

Ganglionic blockers

These drugs act on nicotinic receptors present at autonomic ganglia and can inhibit both sympathetic and parasympathetic transmission. Examples include mecamylamine and hexamethonium.

Individual Drug Pharmacological Actions

Atropine

Atropine is a naturally occurring alkaloid derived from plants like Atropa belladonna. It competitively antagonizes muscarinic receptors, blocking the actions of acetylcholine. Its effects include increased heart rate, bronchodilation, decreased secretions, and relaxation of smooth muscles in the gastrointestinal and genitourinary tracts.

Scopolamine

Scopolamine, also known as hyoscine, is a belladonna alkaloid with similar properties to atropine but has a greater effect on the central nervous system. It is well known for its ability to prevent motion sickness and its use as an antiemetic.

Glycopyrrolate

Glycopyrrolate is a synthetic antimuscarinic agent that has similar effects as atropine but with a longer duration of action and fewer central nervous system side effects.

Mecamylamine

Mecamylamine is a non-competitive antagonist at nicotinic receptors, blocking both sympathetic and parasympathetic transmission at the ganglionic level.

Pharmacological Actions

Central Nervous System

Parasympatholytics can have various effects on the central nervous system (CNS), including sedation, amnesia, and decreased seizure threshold. The intensity of these effects depends on the specific drug and dosage.

Peripheral Nervous System

In the peripheral nervous system, parasympatholytics can inhibit the actions of acetylcholine on smooth muscles, glands, and the heart. This results in decreased gastrointestinal motility, bronchodilation, reduced secretion of salivary, bronchial and gastric glands, and increased heart rate.

Uses

Anesthetic Pre-treatment

Parasympatholytics are often used as a pre-treatment before anesthesia to reduce secretions and prevent bradycardia during surgery.

Ophthalmology

These drugs can cause mydriasis (pupil dilation) and cycloloplegia (paralysis of the ciliary muscle), making them useful for diagnostic and therapeutic procedures in ophthalmology.

Antispasmodic

Parasympatholytics can be used to treat various gastrointestinal and genitourinary spasms, such as irritable bowel syndrome and urinary incontinence.

Bradycardia

These drugs, particularly atropine, can be used to treat bradycardia (slow heart rate) caused by increased vagal tone or certain medications.

Organophosphate Poisoning (OP Poisoning)

Parasympatholytics can be lifesaving in cases of organophosphate poisoning by counteracting the excessive stimulation of cholinergic receptors.

Click here for more details on OP poisoning

Contraindications

Glaucoma

Parasympatholytics are contraindicated in patients with narrow-angle glaucoma or a predisposition to acute angle-closure glaucoma, as they can increase intraocular pressure.

Prostatic Hypertrophy

These drugs should be avoided in patients with prostatic hypertrophy, as they can worsen urinary retention.

Intestinal Obstruction

Parasympatholytics are contraindicated in patients with intestinal obstruction or ileus, as they can further reduce gastrointestinal motility.

Myasthenia Gravis

These drugs should be used with caution in patients with myasthenia gravis, as they can exacerbate muscle weakness.

Tachycardia

Parasympatholytics should be avoided in patients with pre-existing tachycardia or a history of arrhythmias, as they can worsen these conditions.

Adverse Effects

Using parasympatholytics can lead to several side effects, commonly referred to as anticholinergic effects. These may include:

  • Dry mouth
  • Blurred vision
  • Constipation
  • Urinary retention
  • Tachycardia (increased heart rate)
  • Confusion or agitation
  • Drowsiness or dizziness

In severe cases, anticholinergic toxicity can occur, leading to symptoms such as hallucinations, seizures, hyperthermia, and cardiovascular instability.

Atropine Poisoning

Atropine poisoning, also known as anticholinergic poisoning or atropine overdose, can occur following excessive ingestion or administration of atropine or other antimuscarinic agents. Symptoms of atropine poisoning include:

  • Dry, flushed skin
  • Dilated pupils
  • Rapid heart rate
  • Fever
  • Delirium or hallucinations
  • Seizures

Treatment for atropine poisoning includes supportive care, administration of activated charcoal if ingestion is recent, and the use of the antidote physostigmine, which is a cholinesterase inhibitor that increases the levels of acetylcholine.

Click here for more detailed information on Atropine poisoning

Conclusion

Parasympatholytics are a diverse group of drugs that exert their effects by inhibiting the actions of acetylcholine on parasympathetic nerve endings. They have a wide range of clinical applications, but their use should be carefully considered due to potential adverse effects, contraindications, and the risk of atropine poisoning. Understanding the classification, pharmacological actions, and clinical uses of these drugs is essential for healthcare providers to ensure their safe and effective use.

Also, refer to this page for more details.

Cholinergic Antagonists: A Comprehensive Guide to Parasympatholytics and Antimuscarinic Agents

Disclaimer: This article is for informational purposes only and should not be taken as medical advice. Always consult with a healthcare professional before making any decisions related to medication or treatment.

Disclaimer: This article is for informational purposes only and does not constitute medical advice. Always seek the advice of a healthcare provider with any questions regarding a medical condition.

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TAGGED: Anesthetic adjunct, Anticholinergic effects, Anticholinergic toxicity, Anticholinergics, Atropine, Atropine poisoning, Blurred vision, Bradycardia, Cardiovascular disorders, contraindications, Cycloplegia, Dry mouth, Gastrointestinal disorders, Glycopyrrolate, Mecamylamine, Muscarinic receptors, Mydriasis, Neurotransmitter acetylcholine, Nicotinic receptors, Ophthalmic applications, Parasympatholytics, Physostigmine, Scopolamine, Urinary incontinence

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